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Synthesis of (2S,3aR,7aS)-Benzyl Octahydro1H-indole-2-carboxylate

【Author in Chinese】 时涛申杰峰安前进刘德龙刘燕刚张万斌

【Author】 Shi,Taoa Shen,Jiefenga An,Qianjina Liu,Delong,a Liu,Yanganga Zhang,Wanbin,a,b(aSchool of Pharmacy,Shanghai Jiao Tong University,Shanghai 200240)(bSchool of Chemistry and Chemical Engineering,Shanghai Jiao Tong University,Shanghai 200240)

【Institution】 上海交通大学药学院上海交通大学化学化工学院

【Abstract in Chinese】 通过合成路线的改进以及合成工艺的优化,方便高效地得到了抗高血压药物群多普利的关键中间体(2S,3aR,7aS)-八氢-1H-吲哚-2-甲酸苄酯.产品结构及绝对构型通过NMR及HPLC进行表征,与文献报道的数据完全一致.最终以99%的对映选择性及13.2%的产率得到目标化合物.为群多普利关键中间体的合成提供了一条可工业化的途径.

【Abstract】 The key intermediate of antihypertensive drugs trandolapril,(2S,3aR,7aS)-benzyl octahydro-1H-indole-2-carboxylate,was synthesized by improvement of synthetic route and optimation of synthetic technology with satisfactory results(99% ee and 13.2% overall yield).The structure and absolute configuration of the product were characterized by NMR and HPLC analysis,which are completely consistent with the reported data of the literature.It was obvious that the current methodology provided an efficient pathway for the synthesis of trandolapril.

【Fund】 国家自然科学基金(Nos.21172143,21172145,21232004)资助项目~~
  • 【Source】 有机化学 ,Chinese Journal of Organic Chemistry , Editorial E-mail ,2013(07)
  • 【CLC code】TQ463.5
  • 【Internet Publish Date】2013-03-22 17:36
  • 【Downloads】167
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